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Ac-RYYRWK-NH2 TFA

Catalog No. T40510   CAS 408305-09-9
Synonyms: Ac-RYYRWK-NH2 TFA

Ac-RYYRWK-NH2 is a highly effective and specific partial agonist for the nociceptin receptor (NOP). It demonstrates a remarkable affinity for rat cortical membranes ORL1, with [3H]Ac-RYYRWK-NH2 exhibiting a Kd value of 0.071 nM. However, it shows negligible affinity towards μ-, κ-, or δ-opioid receptors.

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Ac-RYYRWK-NH2 TFA Chemical Structure
Ac-RYYRWK-NH2 TFA, CAS 408305-09-9
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Ac-RYYRWK-NH2 is a highly effective and specific partial agonist for the nociceptin receptor (NOP). It demonstrates a remarkable affinity for rat cortical membranes ORL1, with [3H]Ac-RYYRWK-NH2 exhibiting a Kd value of 0.071 nM. However, it shows negligible affinity towards μ-, κ-, or δ-opioid receptors.
In vitro Binding studies with [3H]ac-RYYRWK-NH2 on rat cortical membranes identified a single high-affinity binding site (Kd = 0.071 nM). Furthermore, Naloxone benzoylhydrazone competitively inhibited [3H]ac-RYYRWK-NH2 binding to rat cortical membranes (Ki = 104 nM) and to human ORL1 receptors (Ki = 136 nM). It also displaced [125I]Tyr14-NC-OH binding to ORL1 receptors with a Ki of 37 nM, indicating specificity as it showed no affinity for μ-, κ-, or δ-opioid receptors.
Synonyms Ac-RYYRWK-NH2 TFA
Molecular Weight 1126.21
Formula C51H70F3N15O11
CAS No. 408305-09-9

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keep away from moisture

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. C T Dooley, et al. Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1.J Pharmacol Exp Ther. 1997 Nov;283(2):735-41. 2. M Ho, et al, Characterization of the ORL(1) receptor on adrenergic nerves in the rat anococcygeus muscle. Br J Pharmacol. 2000 Sep;131(2):349-55.

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Keywords

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